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PE20091756A1 - PYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE9A MODULATORS - Google Patents

PYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE9A MODULATORS

Info

Publication number
PE20091756A1
PE20091756A1 PE2009000482A PE2009000482A PE20091756A1 PE 20091756 A1 PE20091756 A1 PE 20091756A1 PE 2009000482 A PE2009000482 A PE 2009000482A PE 2009000482 A PE2009000482 A PE 2009000482A PE 20091756 A1 PE20091756 A1 PE 20091756A1
Authority
PE
Peru
Prior art keywords
alkyl
pde9a
modulators
deficiency
pyrazolopyrimidinone derivatives
Prior art date
Application number
PE2009000482A
Other languages
Spanish (es)
Inventor
Riccardo Giovannini
Cornelia Dorner-Ciossek
Christian Eickmeier
Dennis Fiegen
Thomas Fox
Klaus Fuchs
Niklas Heine
Holger Rosenbrock
Gerhard Schaenzle
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39790395&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20091756(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20091756A1 publication Critical patent/PE20091756A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Anesthesiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN DERIVADO DE PIRAZOLOPIRIMIDINONA DE FORMULA (I), DONDE H ES UN GRUPO HETEROCICLILO DEFINIDO COMO UN SISTEMA DE ANILLOS NO AROMATICO MONOCICLICO, BICICLICO O TRICICLICO, DONDE AL MENOS UNO A TRES DE LOS ATOMOS DE CARBONO ES REEMPLAZADO POR UN HETEROATOMO SELECCIONADO DE N, O O -S(O)r-; R1 ES ALQUILO C1-C8, ALQUENILO C2-C8, ALQUINILO C2-C8, ENTRE OTROS; R2 ES H, -CN, -CF3, ENTRE OTROS; R3 ES H, OH O -OR10; R10 ES H, -CH2-CF3, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R4 Y R5 SON H, FLUOR, ALQUILO C1-C3, ENTRE OTROS; x ES 0 O UN ENTERO DE 1 A 4; y ES 0 O 1; r ES 0, 1 O 2. SON COMPUESTOS PREFERIDOS: (a), (b), (c), ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LA FOSOFDIESTERASA 9A (PDE9A) Y SON UTILES EN EL TRATAMIENTO DE TRANSTORNOS DEL SISTEMA NERVIOSO CENTRAL TALES COMO LA ENFERMEDAD DE ALZHEIMER, DEFICIT DE PERCEPCION, DE APRENDIZAJE O DE MEMORIA, ENTRE OTRASREFERRED TO A PYRAZOLOPYRIMIDINONE DERIVATIVE OF FORMULA (I), WHERE H IS A HETEROCYCLYL GROUP DEFINED AS A NON-AROMATIC SINGLE CYCLIC, BICYCLIC OR TRICYCLIC RING SYSTEM, WHERE AT LEAST ONE TO THREE OF THE HETEROCYCLYL ATOMS IS LISTED N, OO -S (O) r-; R1 IS C1-C8 ALKYL, C2-C8 ALKYL, C2-C8 ALKYL, AMONG OTHERS; R2 IS H, -CN, -CF3, AMONG OTHERS; R3 IS H, OH O -OR10; R10 IS H, -CH2-CF3, C1-C6 ALKYL, C2-C6 ALKYL, AMONG OTHERS; R4 AND R5 ARE H, FLUOR, C1-C3 ALKYL, AMONG OTHERS; x IS 0 OR AN INTEGER FROM 1 TO 4; and ES 0 O 1; r IS 0, 1 OR 2. THE PREFERRED COMPOUNDS ARE: (a), (b), (c), AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE MODULATORS OF PHOSOPHDIESTERASE 9A (PDE9A) AND ARE USEFUL IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS SUCH AS ALZHEIMER'S DISEASE, DEFICIENCY OF PERCEPTION, LEARNING OR MEMORY DEFICIENCY

PE2009000482A 2008-04-02 2009-04-02 PYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE9A MODULATORS PE20091756A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08153987 2008-04-02

Publications (1)

Publication Number Publication Date
PE20091756A1 true PE20091756A1 (en) 2009-12-14

Family

ID=39790395

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2009000482A PE20091756A1 (en) 2008-04-02 2009-04-02 PYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE9A MODULATORS

Country Status (33)

Country Link
US (2) US8623879B2 (en)
EP (1) EP2300478B1 (en)
JP (1) JP5391264B2 (en)
KR (1) KR101623762B1 (en)
CN (1) CN101983199B (en)
AR (1) AR071577A1 (en)
AU (1) AU2009232017B2 (en)
BR (1) BRPI0910690B8 (en)
CA (1) CA2716410C (en)
CL (1) CL2009000800A1 (en)
CO (1) CO6321264A2 (en)
CY (1) CY1117626T1 (en)
DK (1) DK2300478T3 (en)
EA (1) EA021504B1 (en)
EC (1) ECSP10010506A (en)
ES (1) ES2573330T3 (en)
HR (1) HRP20160683T2 (en)
HU (1) HUE027771T2 (en)
IL (1) IL207710A (en)
MA (1) MA32201B1 (en)
ME (1) ME02427B (en)
MX (1) MX2010010821A (en)
MY (2) MY182670A (en)
NZ (1) NZ588245A (en)
PE (1) PE20091756A1 (en)
PL (1) PL2300478T3 (en)
RS (1) RS54724B1 (en)
SG (1) SG189706A1 (en)
SI (1) SI2300478T1 (en)
TW (1) TWI433850B (en)
UA (1) UA105362C2 (en)
UY (1) UY31748A (en)
WO (1) WO2009121919A1 (en)

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